Search Results - "SPALDING, T. A"

The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine by WEINER, D. M, MELTZER, H. Y, VANOVER, K. E, OLSSON, R, JAYATHILAKE, K, LEE, M, LEVEY, A. I, HACKSELL, U, BURSTEIN, E. S, DAVIS, R. E, BRANN, M. R, VEINBERGS, I, DONOHUE, E. M, SPALDING, T. A, SMITH, T. T, MOHELL, N, HARVEY, S. C, LAMEH, J, NASH, N

“…Clozapine is a unique antipsychotic, with efficacy against positive symptoms in treatment-resistant schizophrenic patients, and the ability to improve…”
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5-hydroxytryptamine2A receptor inverse agonists as antipsychotics by Weiner, D M, Burstein, E S, Nash, N, Croston, G E, Currier, E A, Vanover, K E, Harvey, S C, Donohue, E, Hansen, H C, Andersson, C M, Spalding, T A, Gibson, D F, Krebs-Thomson, K, Powell, S B, Geyer, M A, Hacksell, U, Brann, M R

“…We have used a cell-based functional assay to define the pharmacological profiles of a wide range of central nervous system active compounds as agonists,…”
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Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins by Burstein, E S, Spalding, T A, Brann, M R

“…We have examined the effects of raising G protein concentration on the pharmacology of a series of agonist and antagonist ligands at the m1, m3, and m5…”
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Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis by Spalding, T A, Burstein, E S, Brauner-Osborne, H, Hill-Eubanks, D, Brann, M R

“…We have isolated a mutant m5 muscarinic receptor that mediates robust functional responses in the absence of agonists. This constitutively active receptor was…”
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Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins by Burstein, E S, Spalding, T A, Hill-Eubanks, D, Brann, M R

“…To derive structure-function relationships for receptor-G protein coupling, libraries were created of human m5 muscarinic acetylcholine receptors (m5) randomly…”
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Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors by SPALDING, T. A, BIRDSALL, N. J. M, CURTIS, C. A. M, HULME, E. C

“…Acetylcholine mustard (AChM) is an analogue of acetylcholine (ACh) in which the onium headgroup is replaced by a chemically reactive aziridinium moiety. AChM…”
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Constitutive activation of chimeric m2/m5 muscarinic receptors and delineation of G-protein coupling selectivity domains by Burstein, Ethan S., Spalding, Tracy A., Brann, Mark R.

“…To derive structure/function relationships for muscarinic receptor/G-protein coupling, the m2 and m5 muscarinic receptors and a series of m2 m5 chimeras were…”
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Interactions of Muscarinic Receptors with the Heterotrimeric G Proteins Gq and G12: Transduction of Proliferative Signals by Burstein, E. S., Bräuner‐Osborne, H., Spalding, T. A., Conklin, B. R., Brann, M. R.

“…: The proliferative and transforming properties of m2 and m5 muscarinic acetylcholine receptors and a series of wild‐type, chimeric, and mutant G proteins were…”
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The Second Intracellular Loop of the m5 Muscarinic Receptor Is the Switch Which Enables G-protein Coupling by Burstein, Ethan S., Spalding, Tracy A., Brann, Mark R.

“…We have completed a systematic search of the intracellular loops of a muscarinic acetylcholine receptor for domains that govern G-protein coupling. A unique…”
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Allosteric modulation of G-protein coupled receptors by Jensen, Anders A, Spalding, Tracy A

“…The superfamily of G-protein coupled receptors (GPCRs) has more than 1000 members and is the largest family of proteins in the body. GPCRs mediate signalling…”
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Identification of a Ligand-dependent Switch within a Muscarinic Receptor by Spalding, Tracy A., Burstein, Ethan S., Henderson, Shaw C., Ducote, Karin R., Brann, Mark R.

“…G-protein-coupled receptors spontaneously switch between active and inactive conformations. Agonists stabilize the active conformation, whereas antagonists…”
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Functional importance of the Ala(116)-Pro(136) region in the calcium-sensing receptor. Constitutive activity and inverse agonism in a family C G-protein-coupled receptor by Jensen, A A, Spalding, T A, Burstein, E S, Sheppard, P O, O'Hara, P J, Brann, M R, Krogsgaard-Larsen, P, Bräuner-Osborne, H

“…The calcium-sensing receptor (CaR) belongs to family C of the G-protein-coupled receptor superfamily. To date 14 activating mutations in CaR showing increased…”
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Constitutively active muscarinic receptors by Spalding, Tracy A., Burstein, Ethan S.

“…Mutations that increase constitutive activity and alter ligand binding have been used to investigate the structure and mechanism of activation of muscarinic…”
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Constitutive Activation of the m5 Muscarinic Receptor by a Series of Mutations at the Extracellular End of Transmembrane 6 by Spalding, Tracy A, Burstein, Ethan S, Wells, James W, Brann, Mark R

“…The m5 muscarinic acetylcholine receptor was constitutively activated by a wide range of amino acid substitutions at a residue (serine 465) that is positioned…”
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Structure/Function Relationships of a G-Protein Coupling Pocket Formed by the Third Intracellular Loop of the m5 Muscarinic Receptor by Burstein, Ethan S, Spalding, Tracy A, Brann, Mark R

“…Using random saturation mutagenesis, we have previously identified the amino acids K439, A440, and A441 in the C-terminus of the third intracellular loop (Ci3)…”
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Structure of a G-protein-coupling Domain of a Muscarinic Receptor Predicted by Random Saturation Mutagenesis (∗) by Hill-Eubanks, David, Burstein, Ethan S., Spalding, Tracy A., Bräuner-Osborne, Hans, Brann, Mark R.

“…The third intracellular loop (i3) plays a critical role in the coupling of many receptors to G-proteins. In muscarinic receptor subtypes, the N- and C-terminal…”
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Amino acid side chains that define muscarinic receptor/G-protein coupling. Studies of the third intracellular loop by Burstein, E S, Spalding, T A, Brann, M R

“…Amino acids in the third intracellular loops of receptors play pivotal roles in G-protein coupling. To define their structural requirements, we have subjected…”
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Use of random-saturation mutagenesis to study receptor-G protein coupling by Burstein, E S, Spalding, T A, Brann, M R

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Blockade of muscarinic receptors by alkylating agonist analogues by Hulme, E C, Spalding, T A, Curtis, C A, Birdsall, N J, Corrie, J E

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Constitutive activation of muscarinic receptors by the G‐protein Gq by Burstein, Ethan S., Spalding, Tracy A., Braüner-Osborne, Hans, Brann, Mark R.

“…In the absence of ligands, G‐protein coupled receptors interconvert between active and inactive conformations. These conformations are stabilized by agonists…”
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